What is tibolone – and is it a SPEAR?

  title={What is tibolone – and is it a SPEAR?},
  author={D. Purdie},
  pages={236 - 239}
A strange and remarkable beast is among us. Structurally, it is a steroid. Functionally, however, although there are five groupings of steroids, it would appear to belong to none. It is frequently classed, listed and described as a hormone replacement therapy (HRT) preparation, but it is not an estrogen. It has progestogenic and androgenic properties, yet is neither a progestogen nor an androgen, and nor, for good measure, is it a glucocorticoid or a mineralocorticoid. It is artificial in its… Expand
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Topics from this paper

Sulfation of tibolone and tibolone metabolites by expressed human cytosolic sulfotransferases
Tibolone is an important therapeutic agent used in the treatment of menopausal symptoms in many countries and has beneficial effects on menopausal and postmenopausal vasomotor, bone, vaginal and moodExpand
Pros and cons of existing treatment modalities in osteoporosis: a comparison between tibolone, SERMs and estrogen (±progestogen) treatments
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Tibolone: a steroid with a tissue-specific mode of action
  • H. Kloosterboer
  • Medicine, Biology
  • The Journal of Steroid Biochemistry and Molecular Biology
  • 2001
It is concluded that tibolone acts as a tissue-specific compound by mediating its effects via steroid receptors and enzymatic pathways, and avoids stimulation of the endometrium and breast tissue. Expand
The effects of tibolone.
  • J. Rymer
  • Medicine
  • Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
  • 1998
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Org OD 14 and the endometrium.
Long-term therapy with (7 alpha,17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14; tibolone, Livial) has no influence on the endometrium in post-menopausal women. This wasExpand
Tibolone: influence on markers of cardiovascular disease.
The overall effect on hemostatic factors of the present doses of tibolone in healthy, late postmenopausal women tends towards increased fibrinolysis and unchanged coagulation, which may be beneficial and might theoretically counterbalance the potentially negative effect of the decrease in high density lipoprotein cholesterol. Expand
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The inhibition provoked by these steroids on the enzymes involved in the local biosynthesis of the biologically active estrogen estradiol, may reduce the risk of breast cancer in postmenopausal women during long-term hormone replacement treatment with Livial. Expand
Effects of long-term Org OD 14 administration on blood coagulation in climacteric women.
No significant difference was found between the effects of Org OD 14 and placebo with regard to any clotting factors at any time interval, although factor VII and factor X levels were consistently lower in the OD 14 group than in the placebo group. Expand
In vitro evaluation of estrogenic, estrogen antagonistic and progestagenic effects of a steroidal drug (Org OD-14) and its metabolites on human endometrium.
The estrogenic and progestagenic actions of these compounds are in general agreement with their relative affinity for binding to the estradiol and progesterone receptors, although their actions may be influenced by intracellular metabolism in the endometrial tissue. Expand
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Findings indicate that Org OD 14 displays no adverse effects on coagulation, while changes in fibrinolysis seem to be beneficial for post-menopausal women. Expand
The effect of the synthetic steroid Org OD14 on fibrinolysis and blood lipids in postmenopausal women.
Two groups of postmenopausal women were compared and the Org OD14 group showed the following significant differences: higher haemoglobin, haematocrit, platelet count, plasminogen, fibrinolytic activity on fibrin plates and antithrombin III and lower fibr inogen. Expand